Synthetic chalcones as efficient inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase PtpA.
In the search for lead compounds for new drugs for tuberculosis, the activity of 38 synthetic chalcones were assayed for their potential inhibitory action towards a protein tyrosine phosphatase from Mycobacterium tuberculosis--PtpA. The compounds were obtained by aldolic condensation between aldehydes and acetophenones, under basic conditions. Five compounds presented moderate or good activity. The structure-activity analysis reveals that the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents.
Chiaradia
Louise Domeneghini
LD
Departamento de Química, Universidade Federal de Santa Catarina, Campus Trindade, 88040-900 Florianópolis, SC, Brazil.
Mascarello
Alessandra
A
Purificação
Marcela
M
Vernal
Javier
J
Cordeiro
Marlon Norberto Sechini
MN
Zenteno
María Emilia
ME
Villarino
Andréa
A
Nunes
Ricardo José
RJ
Yunes
Rosendo Augusto
RA
Terenzi
Hernán
H
D001426:Bacterial Proteins; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000201:enzymology*; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000235:genetics; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
D001426:Bacterial Proteins; D047188:Chalcones; C414465:MptpA protein, Mycobacterium tuberculosis; D017027:Protein Tyrosine Phosphatases